Bahan Baku Fraksi Diterpen Lakton Herba Sambiloto sebagai Antimalaria

Sambiloto adalah lanaman yang banyak ditemukan di Indonesia. Sambiloto dikelahui memiliki kandungan beragam senyawa diterpen lakton terutama andrografolida dan senyawa flavonoj-d. Andrografolida merupakan senyawa diterpen lakton yang diketahui mempunyai banyak aktivitas yang telah ditunjukkan dan dibuktikan bahwa andrografolida menghambat pertumbuhan P. berghei secara in vivo dan P,falciparun secara jn vitro dengan mekanisme penghambatan pada stadi.um skizon dan gametosit. Sedangkan sambiloto telah lama dimanfaatkan sebagai bahan ramuan obat traditionat untuk mengobati berbagai penyakit termasuk malaria. para penemu dari invensi ini telah menemukan bahwa Fraksi DTL herba sambiloto dapat dijadikan sediaan obat, untuk menqobati penyakit malaria

The Development of tablet formulation of Artocarpus champeden Stembark extract as antimalarial drug

Parasite resistance to antimalarial drug, chloroquine and sulfadoxin-pirimetamin, still e major problem in malaria control worldwide, thereforc, the cffort in developing a new targct of antimalarial drug become a high priority. Our preliminary test revealed that fuom A. chanpeden exhibiedt potent antimalarial activities againts P. lalciparum in vitro brghci in vivo. Several isolaEd compounds from this plant exhibited antimalarial activity drc isotated compound identified as hetcroflavon C, a prenylated flavooe, have a higher activity than chloroquine. Therefore, it is potential to be developed as antimalarial rcscarch was conducted to develop tablet formulation of ethanol extract of A. stcmbark (EEAC). The formula that composed: EEAC 150 mg, lactose 140 mg, cabarnilum 46 mg, avicel PH l0l 79o, primogcl 57o, and Mg stcarat 1% was the selected Th€ tablet hardness o[ the formula has span betwccn 9.0-12.27 kP and the averagc is , thc disintegration time of formula 12 minutcs 4? seconds. A standard fiays test oll P. infected mice was used to evaluated in vrv, antimalarial activity of the tablet. This rlvcalcd that EEAC tablet has antimalarial activity against parasite P. berghei in vivo. ration ofEEAC tablet at a dose of 10 mg/kg body weight multiple dose (twice a day) thc parasite growth better than 100 mg/kg body weight single dose (once a day) activity of tablet in multiple dose pcr oral shqwed inhibition of parasite growth of while at single dose per oral showed inhibition of parasite growth of 83.32

Dissolution Enhancement of Gendarusin A by Poloxamer 188 Addition in Justicia gendarussa Burm. f Ethanolic Extract Granule Matrix

Justicia gendarussa Burm. f (Acanthaceae) is often used as folk medicine for many purposes in Indonesian indigenous tribes. Preclinical studies on J. gendarussa leaves indicated that the extract possessed the activity of male contraception. Gendarusin A was found to be the compound responsible for the activity. The purpose of this study was to prove that poloxamer 188 can increase the dissolution rate of gendarusin A in Justicia gendarussa Burm. f ethanolic extract granule (JEG) matrix, in an effort to find male contraceptives phytopharmaceutical product. In this research, we had made three JEG matrix types, which were type 1 (without the addition of surfactant poloxamer 188); type 2 (with the addition of 1% surfactant poloxamer 188), and type 3 (with the addition of 2% surfactant poloxamer 188). The three types of JEG matrix then examined by dissolution test to obtain the dissolution rate of gendarusin A. HPLC instrument was utilized to analyse the concentration of gendarusin A from dissolution mediums. The results showed that the gendarusin A in JEG matrix type 3 dissolved much faster compared to JEG matrix type 1 and type 2. The score of dissolution efficiencies of gendarusin A in JEG matrix type 1, type 2, and type 3 were 15,72%; 24,22%; and 31,83% respectively. It can be concluded that poloxamer 188 addition can increase the dissolution rate of gendarusin A in JEG matrix

In vivo antimalarial activity of Andrographis paniculata Tablets

The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four consecutive days of the AP fractions product, which were Tablet I: wet granulated formula of AP fraction A; Tablet II: wet granulated formula of AP fraction B; Tablet III: solid dispersion formula of AP fraction B.. The results revealed that three phytopharmaceutical products of A.paniculata were inhibited parasite's growth with inhibition range of 70.15% to 80.35%. There was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A. paniculata active substance

KINETICS STUDY COCRYSTALS KETOCONAZOLE-SUCCINIC ACID PREPARED WITH SLURRY METHOD BASED ON POWDER X-RAY DIFFRACTION (PXRD)

The compounds with low solubility drugs can be a problem in the development of drugs for the pharmaceutical industry. Group of drugs that are included in the Biopharmaceutical Classification System (BCS) class II drugs can be a challenge for the preparations of pharmaceutical development because of low solubility drugs as well as the rate of dissolution. In this case to increase the solubility of drugs besides salts, pharmaceutical cocrystals opened a new dimension to search for solid forms such as solubility, dissolution rate, stability, and shelf life of active pharmaceutical ingredients (APIs) without affecting their inherent pharmacological properties1. Pharmaceutical co crystals are materials or crystalline materials consisting of at least two different components (multicomponent crystals or mixed crystals)2-3. Co crystal could be prepared by several methods, such as solvent evaporation, slurry, melt, and grinding. Co crystals formed between ketoconazole (KTZ) as an active pharmaceutical and succinic acid (SA) as a co crystal former (co-former)4 was increased dissolution rate of pure ketoconazole in equimolar ratio (1:1)1. Physical characterization of co crystal was performed by physical mixture of binary system with molar ratio using different thermal analyzer (DTA) data from KTZ and SA. Besides that, physicochemical characterizations of cocrystal were performed by using PXRD and infrared spectroscopy (IR). Active solid materials in the manufacture of pharmaceutical preparation suffered in various thermic or machanical proccessed such as grinding, milling, granulations (wet and dry granulations), tabletasi, and storage at various temperature, so the materials can occure transformation polymorph or hidrat/ solvat5. Kinetic study of cocrystal KTZ-SA prepared with slurry method at various solvent concentrations a follows 2%, 3%, 4%, 5% and 6% (w/w). Therefore, the aim of the present study was determined the kinetics of co crystals KTZ-SA prepared with slurry method by using Powder X-ray Diffraction (PXRD) data such as the research of co crystalline phase transformation of binary mixture of trimethoprim (TMP) and sulfamethoxazol (SMZ) by slurry technique5

In vivo antimalarial activity of Andrographis paniculata Tablets

The formulation of three phytopharmaceutical products of Andrographispaniculata fractions (AP fraction A and B) containing diterpene lactones as an active substance were developed and their antimalarial activities against Plasmodium bergheihas been examined. In vivo antimalarial assay on P. berghei infected mice was carried out by oral administration,twice a dayfor four consecutive days of the AP fractions product, which were Tablet I: wet granulated formula of AP fraction A; Tablet II: wet granulated formula of AP fraction B; Tablet III: solid dispersion formula of AP fraction B.. The results revealed that three phytopharmaceutical products of A.paniculata were inhibited parasite's growth with inhibition range of 70.15% to 80.35%. There was no significant difference of antimalarial activities between Tablet II and III, meanwhile there was significant difference among Tablet I with Tablet II and Tablet III.It was concluded that antimalarial activity depending on raw material form of A. paniculata active substance

Pharmacokinetic Parameters Determination of Gendarusin a in Men Subject Urine After Administration of Ethanol Extract of Justicia Gendarussa Burm. F. Leaf (Ethno Medicine Research)

Justicia gendarussa Burm. f (Famili: Acanthaceae) has flavonoid that inhibits hyaluronidase enzyme of spermatozoa in the fertilization process. Previous research reported that the major component of J.gendarussa was 6,8-di-L-arabinopyranosil- 4’,5,7-trihydroxy flavones or 6,8-diarabinosylapigenin (gendarusin A).Objective: This experimental study has been carried out to determine the pharmacokinetic parameters of gendarusin A in human urine after single oral administration of J.gendarussa extract. Methods: Six healthy men were enlisted in this study. Urine samples were collected at intervals for 24 hours before and after six healthy volunteers administrated orally 100 ml ethanol extract suspension of J. gendarussa leaves, containing 1 g of extract equal to 16,4 mg gendarusin A, for the measurement of gendarusin A by HPLC. Result: The calibration curve of gendarusin A peak areas (y) against the concentrations (x, μg/ml) in urine was linear and the regression equations was y = 34.3496x + 63.6315 (r = 0.9992). The lowest absolute recovery was 106.10 %, while the lowest assay recovery was 81.92 %, which revealed that the accuracy of the method was satisfied. All values of the R.S.D. of intra-day precision were less than 8,12 %. The LOD and LOQ of assaying gendarusin A in urine was 0.0817 μg/ml and 0.2724 μg/ml, respectively. Conclusion: Following oral administration of J.gendarussa extract suspension, the result show that the elimination half-lives (t ½) for gendarusin A in the urinary excretion were 2,44 – 8,53 hours (mean 4,44 ± 2,14 hours) and the rates constant of elimination (Kel) were 0,08 – 0,28 hour-1 (mean 0,18 ± 0,07 hour-1)

Peningkatan kelarutan dan bioavailabilitas kurkumin (Curcuma Xanthoriza Linn) dengan membentuk senyawa inklusi kurkumin-hidroksipropil-B-siklodekstrin

Tujuan penelitian ini adalah untuk memperbaiki kelarutan dan meningkatkan disolusi serta bioavailabilitas kurkumin. Kurkumin adalah bahan baku yang diperoleh dari rimpang temu lawak (Curcumin xanthoriza Linn) yang aktifitas terapinya cukup luas, praktis tidak lamt dalam air dan bioavailabilitasnya rendah. Penelitian yang sekarang dilakukan adalah membuat kompleksasi inklusi antara kurkumin dan HP~CD. Kompleks kurkumin-HP~CD disiapkan dengan cara koevaporasi, sementara campuran fisik diperoleh dengan pencampuran sederhana. Analisis kelarutan setimbang dilakukan untuk menentukan konstante stabilitas kompleks inklusi. Studi kelarutan fase menunjukkan diagram tipe AL dengan kompleksasi perbandingan molar 1 : 1 dan konstante stabilitasnya 30,09 mM-I. Kompleks inklusi padat ini selanjutnya dikarakterisasi dengan DTA, difraksi sinar-X, SEM dan FTIR. Analisis DTA dan difraksi sinar-X menunjukkan bahwa kurkumin berada sebagai bentuk kompleks amorf dalam kompleks koevaporasi. Studi disolusi menunjukkan bahwa kurkumin berada dalam kompleks terkoevaporasi yang disolusinya lebih besar daripada kurkumin murni dan campuran fisiko Temuan penelitian ini memberi bukti kurkumin berhasil ditingkatkan disolusi dan kemungkinan bioavailabilitasnya

Peningkatan kelarutan dan bioavailabilitas kurkumin (Curcuma Xanthoriza Linn) dengan membentuk senyawa inklusi kurkumin-hidroksipropil-B-siklodekstrin

Tujuan penelitian ini adalah untuk memperbaiki kelarutan dan meningkatkan disolusi serta bioavailabilitas kurkumin. Kurkumin adalah bahan baku yang diperoleh dari rimpang temu lawak (Curcumin xanthoriza Linn) yang aktifitas terapinya cukup luas, praktis tidak lamt dalam air dan bioavailabilitasnya rendah. Penelitian yang sekarang dilakukan adalah membuat kompleksasi inklusi antara kurkumin dan HP~CD. Kompleks kurkumin-HP~CD disiapkan dengan cara koevaporasi, sementara campuran fisik diperoleh dengan pencampuran sederhana. Analisis kelarutan setimbang dilakukan untuk menentukan konstante stabilitas kompleks inklusi. Studi kelarutan fase menunjukkan diagram tipe AL dengan kompleksasi perbandingan molar 1 : 1 dan konstante stabilitasnya 30,09 mM-I. Kompleks inklusi padat ini selanjutnya dikarakterisasi dengan DTA, difraksi sinar-X, SEM dan FTIR. Analisis DTA dan difraksi sinar-X menunjukkan bahwa kurkumin berada sebagai bentuk kompleks amorf dalam kompleks koevaporasi. Studi disolusi menunjukkan bahwa kurkumin berada dalam kompleks terkoevaporasi yang disolusinya lebih besar daripada kurkumin murni dan campuran fisiko Temuan penelitian ini memberi bukti kurkumin berhasil ditingkatkan disolusi dan kemungkinan bioavailabilitasnya